Evidence map›Paper›PMID 32727014›Full record

ArticlePharmaceutics2020

Fasudil Loaded PLGA Microspheres as Potential Intravitreal Depot Formulation for Glaucoma Therapy.

Raphael Mietzner, Christian Kade, Franziska Froemel, Diana Pauly, W Daniel Stamer, Andreas Ohlmann, Joachim Wegener, Rudolf Fuchshofer, Miriam Breunig

Open access · goldAbstract read
In one paragraph

Article in Pharmaceutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
29citing papers in PubMed, 1 pooled it
2.9field-weighted citation impact, top 8% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

29 citing papers in PubMed, 1 synthesis or guideline pooled it, 42 citations in OpenAlex.

  1. Pooled it
  2. Article
  3. Article
  4. Article
  5. Review
  6. Review
  7. Review
  8. Current perspectives in tackling glaucoma blindness.Indian journal of ophthalmology · 2025
    Review
  9. Article
  10. Review
  11. Article
  12. Review
  13. Review
  14. Review
  15. The Application of Rho Kinase Inhibitors in the Management of Glaucoma.International journal of molecular sciences · 2024
    Review
  16. Article
  17. Article
  18. Review
  19. The Role of Rho Kinase Inhibitors in Corneal Diseases.Drug design, development and therapy · 2024
    Review
  20. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 5 institutions in 2 countries.

Raphael MietznerDepartment of Pharmaceutical Technology, University of Regensburg, Universitaetsstrasse 31, 93040 Regensburg, Germany.ORCID 0000-0002-1064-9087
Christian KadeInstitute of Analytical Chemistry, Chemo- and Biosensors, University of Regensburg, Universitaetsstrasse 31, 93040 Regensburg, Germany.
Franziska FroemelDepartment of Human Anatomy and Embryology, University of Regensburg, Universitaetsstrasse 31, 93040 Regensburg, Germany.
Diana PaulyExperimental Ophthalmology, University Hospital Regensburg, Franz Josef Strauss Allee 11, 93053 Regensburg, Germany.ORCID 0000-0002-1563-1601
W Daniel StamerDepartment of Ophthalmology, Duke University, Durham, NC 27710, USA.
Andreas OhlmannDepartment of Ophthalmology, Ludwig-Maximilians-University Munich, Mathildenstrasse 8, 80336 Munich, Germany.
Joachim WegenerInstitute of Analytical Chemistry, Chemo- and Biosensors, University of Regensburg, Universitaetsstrasse 31, 93040 Regensburg, Germany.
Rudolf FuchshoferDepartment of Human Anatomy and Embryology, University of Regensburg, Universitaetsstrasse 31, 93040 Regensburg, Germany.
Miriam BreunigDepartment of Pharmaceutical Technology, University of Regensburg, Universitaetsstrasse 31, 93040 Regensburg, Germany.ORCID 0000-0002-1320-6820
University of Regensburg · DEDuke University · USFraunhofer Research Institution for Microsystems and Solid State Technologies · DELudwig-Maximilians-Universität München · DEUniversity Hospital Regensburg · DE

Funding

eNOS-Dependent Mechanoregulation of Intraocular PressureR01EY022359 · NEI · DUKE UNIVERSITY · PI STAMER, W DANIEL · 2012 to 2025
$5.6M
Deutsche Forschungsgemeinschaft BR3566/3-1Deutsche Forschungsgemeinschaft FU734/4-1NEI NIH HHS R01 EY022359NIH HHS EY019696NIH HHS EY022359
6 · The paper itself

Abstract

Rho-associated protein kinase (ROCK) inhibitors allow for causative glaucoma therapy. Unfortunately, topically applied ROCK inhibitors suffer from high incidence of hyperemia and low intraocular bioavailability. Therefore, we propose the use of poly (lactide-co-glycolide) (PLGA) microspheres as a depot formulation for intravitreal injection to supply outflow tissues with the ROCK inhibitor fasudil over a prolonged time. Fasudil-loaded microspheres were prepared by double emulsion solvent evaporation technique. The chemical integrity of released fasudil was confirmed by mass spectrometry. The biological activity was measured in cell-based assays using trabecular meshwork cells (TM cells), Schlemm's canal cells (SC cells), fibroblasts and adult retinal pigment epithelium cells (ARPE-19). Cellular response to fasudil after its diffusion through vitreous humor was investigated by electric cell-substrate impedance sensing. Microspheres ranged in size from 3 to 67 µm. The release of fasudil from microspheres was controllable and sustained for up to 45 days. Released fasudil reduced actin stress fibers in TM cells, SC cells and fibroblasts. Decreased collagen gel contraction provoked by fasudil was detected in TM cells (~2.4-fold), SC cells (~1.4-fold) and fibroblasts (~1.3-fold). In addition, fasudil readily diffused through vitreous humor reaching its target compartment and eliciting effects on TM cells. No negative effects on ARPE-19 cells were observed. Since fasudil readily diffuses through the vitreous humor, we suggest that an intravitreal drug depot of ROCK inhibitors could significantly improve current glaucoma therapy particularly for patients with comorbid retinal diseases.

Indexed as

drug deliveryElectric Cell-Substrate Impedance Sensingfasudilglaucomaintravitreal injectionPLGA microspheresretinal pigment epitheliumROCK inhibitorSchlemm’s canaltrabecular meshwork

Identifiers

PMID32727014
PMCPMC7464914
OpenAlexW3046196587

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.